SAR-405是一种选择性 PIK3C3/Vps34 抑制剂,IC50为1.2 nM,Kd 为1.5 nM,可防止自噬并与肿瘤细胞中的 MTOR 抑制协同作用。它抑制饥饿或 mTOR 抑制诱导的自噬,具有抗癌活性。 SAR-405 is a potent and selective PIK3C3/Vps34 inhibitor (IC50:1.2 nM; Kd:1.5 nM) that prevents autophagy and synergizes with MTOR inhibition in tumor cells. SAR405 treatment also inhibits autophagy induced either by starvation or by MTOR (mechanistic target of rapamycin) inhibition. Combining SAR405 with everolimus results in a significant synergy on the reduction of cell proliferation using renal tumor cells.
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SAR-405
CAS number:1523406-39-4 molecular formula:C19H21ClF3N5O2
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| Chinese alias | (S)-9-((5-氯吡啶-3-基)甲基)-2-((R)-3-甲基吗啉)-8-(三氟甲基)-6,7,8,9-四氢-4H-嘧啶并[1,2-a]嘧啶-4-酮 | ||
| English alias | (S)-9-((5-Chloropyridin-3-yl)methyl)-2-((R)-3-methylmorpholino)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one | ||
| CAS number | 1523406-39-4 | molecular formula | C19H21ClF3N5O2 |
| molecular weight | 443.85 g/mol | Exact mass | - |
| PSA | 61.300 Ų | logp | 2.200 |
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